Download Is PF-232798 a possible successor to maraviroc?

From TreatmentUpdate 166
Is PF-232798 a possible successor to maraviroc?
Maraviroc (Celsentri) is the first of a new family or class of anti-HIV medicines called entry inhibitors. Maraviroc
works by blocking an important receptor, called CCR5, found on the surface of cells. By blocking or covering up this
receptor, maraviroc prevents HIV from entering and infecting the cell.
When taken as part of HAART, maraviroc can suppress viral loads and raise CD4+ cell counts. The drug is taken
twice daily.
Scientists working for the pharmaceutical company Pfizer have developed a new CCR5 receptor blocker. For now,
the compound only has a strange designation—PF-232798.
In lab experiments, the new entry inhibitor stops HIV from entering cells. It may have potential anti-HIV activity
against strains of HIV resistant to maraviroc.
So far, limited studies have been conducted with this compound and they suggest in the short-term the following:
PF-232798 is well absorbed
a dose of 250 mg once daily results in high and sustained anti-HIV levels in the blood
the drug is well tolerated at the 250 mg dose
A more detailed study to assess the effectiveness of PF-232798 has been conducted in Germany with symptomfree HIV positive people. However, Pfizer is analyzing the results, which are not yet publicly available.
If the news on PF-232798 is promising, further trials of this drug will be forthcoming.
REFERENCE:
Dorr P, M Westby, L McFadyen, et al. PF-232798, a second generation oral CCR5 antagonist. Program and abstracts
of the 15th Conference on Retroviruses and Opportunistic Infections , 3-6 February 2008, Boston, MA. Abstract
737.
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